Chemical Name: 4-Methyl-5-(2-pyrazinyl)-3H-1,2-dithiole-3-thione
Biological ActivityOltipraz is a Nrf2 activator; activates Nrf, which binds to antioxidant response elements (AREs) and induces Phase-I and -II drug-metabolizing enzymes including CYP2B and NQO1. Also increases mRNA levels of multiple hepatic xenobiotic transporters. Elevates expression of genes encoding anti-oxidant and multidrug resistance-associated proteins. Displays chemopreventive activity.
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Induction of Nrf2-regulated genes by 3H-1, 2-dithiole-3-thione through the ERK signaling pathway in murine keratinocytes.
Manandhar et al.
Eur J Pharmacol., 2007;577:17
Oxidative and electrophilic stress induces multidrug resistance-associated protein transporters via the nuclear factor-E2-related factor-2 transcriptional pathway.
Maher et al.
Induction of drug metabolism enzymes and transporters by oltipraz in rats.
Merrell et al.
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